Process for the borylation of organohalides

Abstract

The present invention relates to a process for the borylation of organohalides.

1 - 9 . (canceled) 
     
     
         10 . A process for the preparation of an organoboronic acid ester comprising the step of reacting an organohalide with a diol and tetrahydroxydiboron or tetrakis(dimethylamino)diboron in the presence of a transition metal catalyst and a base. 
     
     
         11 . The process according to  claim 10 , wherein the diol is ethylene glycol, 1,2-propanediol, 1,3-propanediol, 1,3-butanediol, 2-methyl-2,4-pentanediol, pinacol or neopentyl glycol. 
     
     
         12 . The process according to  claim 10 , wherein the base is potassium acetate, sodium acetate, lithium acetate, potassium phosphate, sodium phosphate, lithium phosphate, potassium carbonate, sodium carbonate, lithium carbonate, trimethylamine or triethylamine. 
     
     
         13 . The process according to  claim 10 , wherein the transition metal catalyst comprises a Group 8 metal of the Periodic Table. 
     
     
         14 . The process according to  claim 10 , wherein the transition metal catalyst comprises one or more phosphine ligands. 
     
     
         15 . The process according to  claim 10 , wherein the transition metal catalyst is a palladium phosphine complex. 
     
     
         16 . The process according to  claim 10 , wherein the organohalide is an aryl or heteroaryl halide. 
     
     
         17 . The process according to  claim 10 , wherein all components are combined before the entire mixture is heated to the desired reaction temperature. 
     
     
         18 . A process for cross-coupling of two organohalides, comprising the preparing the organoboronic acid ester according to  claim 10  followed directly by the addition of a second organohalide.